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ABT-724

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Chemical Structure| 70006-24-5 同义名 : -
CAS号 : 70006-24-5
货号 : A1000642
分子式 : C17H19N5
纯度 : 98%+
分子量 : 293.366
MDL号 : MFCD05262347
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 Dopamine is the main catecholamine in the central nervous system. The dopamine D4 receptor is abundantly expressed in the cortex and hypothalamus, and plays a key role in the regulation of sexual function in mammals. ABT-724 is a highly potent, selective dopamine D4 receptor with an EC50 value of 12.4nM and 61% efficacy for human dopamine D4 receptor, but shows no effect on dopamine D1, D2, D3, or D5 receptors. ABT-724 also exhibits potent but partial agonist effects on rat and ferret D4 receptors with EC50 values of 14.3±0.6nM and 23.2±1.3nM, respectively. Subcutaneous injection of ABT-724 at doses of 0.01, 0.03, 0.1, 0.3, and 1μmol/kg induced significant facilitation of penile erection in rats. The maximal effect was observed at 0.03μmol/kg with a 77% incidence, compared to 23% incidence in the control group. The latency to induce a penile erection in ABT-724-treated rats was 18.7 minutes. Also in rats with chronically implanted cannulas, injection of ABT-724 directly into the lateral ventricle significantly facilitated erectile responses at 3nmol. Subcutaneous administration of ABT-724 at 0.0025μmol/kg resulted in 2.0±0.6 episodes of increase in intracavernous pressure in an awake freely moving rat.[1]
作用机制 ABT-724 is a selective dopamine D4 receptor agonist that facilitates penile erection in rats without affecting cardiovascular, gastrointestinal, or central nervous system function.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.41mL

0.68mL

0.34mL

17.04mL

3.41mL

1.70mL

34.09mL

6.82mL

3.41mL

参考文献

[1]Brioni JD, Moreland RB, Cowart M, Hsieh GC, Stewart AO, Hedlund P, Donnelly-Roberts DL, Nakane M, Lynch JJ 3rd, Kolasa T, Polakowski JS, Osinski MA, Marsh K, Andersson KE, Sullivan JP. Activation of dopamine D4 receptors by ABT-724 induces penile erection in rats. Proc Natl Acad Sci U S A. 2004 Apr 27;101(17):6758-63. doi: 10.1073/pnas.0308292101